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ALX-350-006 Revised 05-Apr-08
Genistein (synthetic)
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SYNONYMS 4',5,7-Trihydroxyisoflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-006-M010   10 mg 25.00 USD Add To Cart
ALX-350-006-M025   25 mg 50.00 USD Add To Cart
ALX-350-006-M050   50 mg 90.00 USD Add To Cart
ALX-350-006-M100   100 mg 150.00 USD Add To Cart
ALX-350-006-G001   1 g 480.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 446-72-0
MERCK INDEX: 14: 4391
RTECS: NR2392000
SOURCE/HOST: Synthetic.
PURITY: ≥99% (HPLC)
APPEARANCE: White to yellow crystalline powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Tyrosine protein kinase inhibitor. Inhibits phosphorylation of EGFR kinase. Inhibits tumor cell proliferation and induces tumor cell differentiation. Inhibits topoisomerase II activity in vivo. Produces cell cycle arrest and apoptosis. Direct inhibitor of insulin-induced glucose uptake in adipocytes (IC50=20µM).
Product Specific Literature References
Genistein, a specific inhibitor of tyrosine-specific protein kinases: T. Akiyama, et al.; J. Biol. Chem. 262, 5592 (1987) Abstract; Full Text
Erbstatin blocks platelet activating factor-induced protein-tyrosine phosphorylation, polyphosphoinositide hydrolysis, protein kinase C activation, serotonin secretion and aggregation of rabbit platelets: H. Salari, et al.; FEBS Lett. 263, 104 (1990) Abstract
Mechanisms of cancer chemoprevention by soy isoflavone genistein: F.H. Sarkar & Y. Li; Cancer Metastasis Rev. 21, 265 (2002) Abstract
Soy isoflavone phyto-pharmaceuticals in interleukin-6 affections. Multi-purpose nutraceuticals at the crossroad of hormone replacement, anti-cancer and anti-inflammatory therapy: N. Dijsselbloem, et al.; Biochem. Pharmacol. 68, 1171 (2004), Review Abstract
Genistein affects testosterone secretion by Leydig cells in roosters (Gallus gallus domesticus): M. Opalka, et al.; Reprod. Biol. 4, 185 (2004) Abstract
Genistein directly inhibits GLUT4-mediated glucose uptake in 3T3-L1 adipocytes: M. Bazuine, et al.; BBRC 325, 511 (2005) Abstract
Decreased circulating levels of tumor necrosis factor-alpha in postmenopausal women during consumption of soy-containing isoflavones: Y. Huang, et al.; J. Clin. Endocrinol. Metab. 90, 3956 (2005) Abstract
Phytoestrogens and lipoproteins in women: C.N. Bairey Merz, et al.; J. Clin. Endocrinol. Metab. 91, 2209 (2006) Abstract
Clinical review: a critical evaluation of the role of soy protein and isoflavone supplementation in the control of plasma cholesterol concentrations: A. Dewell, et al.; J. Clin. Endocrinol. Metab. 91, 772 (2006), Review Abstract
The role of genistein and synthetic derivatives of isoflavone in cancer prevention and therapy: F.H. Sarkar, et al.; Mini Rev. Med. Chem. 6, 401 (2006), Review Abstract
 
 
ALX-350-008 Revised 02-Oct-07
Chelerythrine chloride
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SYNONYMS 1,2-Dimethoxy-N-methyl-[1,3]benzodioxolo[5,6-c]phenanthridinium chloride
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-008-M001   1 mg 25.00 USD Add To Cart
ALX-350-008-M005   5 mg 75.00 USD Add To Cart
ALX-350-008-M025   25 mg 300.00 USD Add To Cart
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Product Specification
FORMULA: C21H18NO4Cl
MW: 383.8
CAS NUMBER: 3895-92-9
MERCK INDEX: 14: 2051
RTECS: FL9200000
SOURCE/HOST: Synthetic.
PURITY: ≥97% (completely free of biologically active impurities, such as sanguinarine)
APPEARANCE: Yellow to orange solid.
SOLUBILITY: Soluble in DMSO, water, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Heating to 40-50°C with gentle agitation may support complete solubilization. Further dilute with buffer just prior to use. Stock solutions should be refrigerated or frozen between for storage.
HAZARD: HARMFUL.

Product Description
Potent, selective and cell permeable protein kinase C (PKC) inhibitor. Induces apoptosis. BH3 mimetic which inhibits Bcl-XL function.
Product Specific Literature References
Antiplatelet effects of chelerythrine chloride isolated from Zanthoxylum simulans: F.-N. Ko, et al.; Biochim. Biophys. Acta 1052, 360 (1990) Abstract
Chelerythrine is a potent and specific inhibitor of protein kinase C: J.M. Herbert, et al.; BBRC 172, 993 (1990) Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994) Abstract
Identification of chelerythrine as an inhibitor of BclXL function: S.L. Chan, et al.; J. Biol. Chem. 278, 20453 (2003) Abstract
Chelerythrine and sanguinarine dock at distinct sites on BclXL that are not the classic BH3 binding cleft: Y.H. Zhang, et al.; J. Mol. Biol. 364, 536 (2006) Abstract
The effect of chelerythrine on cell growth, apoptosis, and cell cycle in human normal and cancer cells in comparison with sanguinarine: J. Malikova, et al.; Cell Biol. Toxicol. 22, 439 (2006) Abstract
 
 
ALX-350-014 Revised 03-Apr-08
Calyculin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-014-C010   10 µg 65.00 USD Add To Cart
ALX-350-014-C025   25 µg 110.00 USD Add To Cart
ALX-350-014-C050   50 µg 190.00 USD Add To Cart
ALX-350-014-C100   100 µg 320.00 USD Add To Cart
Product Specification
FORMULA: C50H81N4O15P
MW: 1009.2
CAS NUMBER: 101932-71-2
SOURCE/HOST: Isolated from Discodermia calyx.
PURITY: ≥95%
APPEARANCE: Lyophilized.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetonitrile, chloroform, methylene chloride or benzene. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: May by subject to isomerization when in solution. Biological activity is not affected by isomerization.
HANDLING: Protect from light and moisture.
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Potent cell permeable inhibitor with high specificity for protein phosphatase 1 (PP1) and 2A (PP2A). Inhibits p130cas tyrosine phosphorylation. Enhances the phosphorylation level of NF-κB. Affects intracellular signalling processes that require 14-3-3. Potent non-phorbol type tumor promoter. Prevents γ-radiation induced apoptosis.
Product Specific Literature References
Okadaic acid: an additional non-phorbol-12-tetradecanoate-13-acetate- type tumor promoter: M. Suganuma, et al.; PNAS 85, 1768 (1988) Abstract
Protein phosphatases come of age: P.Cohen & P.T. Cohen; J. Biol. Chem. 264, 21435 (1989) Abstract; Full Text
Calyculin A and okadaic acid: inhibitors of protein phosphatase activity: H. Ishihara, et al.; BBRC 159, 871 (1989) Abstract
The structure and regulation of protein phosphatases: P. Cohen; Ann. Rev. Biochem. 58, 453 (1989) Abstract
Calyculin A, an inhibitor of protein phosphatases, a potent tumor promoter on CD-1 mouse skin: M. Suganuma, et al.; Cancer Res. 50, 3521 (1990) Abstract
Nonphorbol tumor promoters okadaic acid and calyculin-A induce membrane translocation of protein kinase C: R. Gopalakrishna; BBRC 189, 950 (1992) Abstract
Comparative effects of protein phosphatase inhibitors (okadaic acid and calyculin A) on human leukemia HL60, HL60/ADR and K562 cells: K. Sakurada, et al.; BBRC 187, 488 (1992) Abstract
Calyculin A, a potent inhibitor of phosphatases-1 and -2A, prevents apoptosis: Q. Song & M.F. Lavin; BBRC 190, 47 (1993) Abstract
Enhancement of AMPA-mediated synaptic transmission by the protein phosphatase inhibitor calyculin A in rat hippocampal slices: A. Figurov, et al.; Eur. J. Neurosci. 5, 1035 (1993) Abstract
Calyculin A, a non-phorbol ester type tumor promotor, induced oxidative DNA damage in stimulated human neutrophil-like cells: T. Takeuchi, et al.; BBRC 205, 1803 (1994) Abstract
Potassium and calcium channel involvement in induction of long-lasting synaptic enhancement by calyculin A, a protein phosphatase inhibitor, in rat hippocampal CA1 region: N. Murakami, et al.; Neurosci. Lett. 176, 181 (1994) Abstract
Differential toxicity of the protein phosphatase inhibitors microcystin and calyculin A: M.T. Runnegar, et al.; J. Pharmacol. Exp. Ther. 273, 545 (1995) Abstract
Inhibition of p130cas tyrosine phosphorylation by calyculin A: W. Qiu, et al.; J. Leukoc. Biol. 63, 631 (1998) Abstract
Unique features of the okadaic acid activity class of tumor promoters: H. Fujiki & M. Suganuma; J. Cancer Res. Clin. Oncol. 125, 150 (1999), Review Abstract
Calyculin A-induced vimentin phosphorylation sequesters 14-3-3 and displaces other 14-3-3 partners in vivo: G. Tzivion, et al.; J. Biol. Chem. 275, 29772 (2000) Abstract
Calyculin A induces apoptosis and stimulates phosphorylation of p65NF-kappaB in human osteoblastic osteosarcoma MG63 cells: H. Tanaka, et al.; Int. J. Oncol. 31, 389 (2007) Abstract
 
 
ALX-350-016 Revised 31-Jul-08
(+)-Aphidicolin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-016-M001   1 mg 65.00 USD Add To Cart
ALX-350-016-M005   5 mg 260.00 USD Add To Cart
ALX-350-016-M025   25 mg 890.00 USD Add To Cart
Product Specification
FORMULA: C20H34O4
MW: 338.5
CAS NUMBER: 38966-21-1
MERCK INDEX: 14: 727
RTECS: PB9185000
SOURCE/HOST: Isolated from Nigrospora oryzae.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (50mg/ml), methanol (10mg/ml) or 100% ethanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Reversible inhibitor of eukaryotic nuclear DNA replication. Useful for cell synchronization. Blocks the cell cycle at early S phase. Prolongs the half life of DNA methyltransferase. Specific inhibitor of DNA polymerase α and δ in eukaryotic cells and in some viruses of animal origin. Acts synergistically with vincristine and doxorubicin. Apoptosis inhibitor/inducer.
Product Specific Literature References
X-Ray crystallographic determination of the structure of the antibiotic aphidicolin: a tetracyclic diterpenoid containing a new ring system: K.M. Brundret, et al.; J. C. S. Chem. Commun. 1027 (1972)
The production of aphidicolin by Nigrospora sphaerica: A.N. Starratt and S.R Loschiavo; Can. J. Microbiol. 20, 416 (1974)
Aphidicolin prevents mitotic cell division by interfering with the activity of DNA polymerase-alpha: S. Ikegami, et al.; Nature 275, 458 (1978) Abstract
Inhibition by aphidicolin of cell cycle progression and DNA replication in sea urchin embryos: S. Ikegami, et al.; J. Cell. Physiol. 100, 439 (1979) Abstract
New views of the biochemistry of eucaryotic DNA replication revealed by aphidicolin, an unusual inhibitor of DNA polymerase alpha: J.A. Huberman; Cell 23, 647 (1981) Abstract
Aphidicolin: a specific inhibitor of nuclear DNA replication in eukaryotes: S. Spadari, et al.; TIBS 7, 29 (1982)
Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in human myeloid leukemia cell lines: K. Kuwakado, et al.; Biochem. Pharmacol. 46, 1909 (1993) Abstract
Life, death and genomic change in perturbed cell cycles: R.T. Schimke, et al.; Philos. Trans. R. Soc. London B Biol. Sci. 345, 311 (1994) Abstract
Dissociation of nuclear and cytoplasmic cell cycle progression by drugs employed in cell synchronization: L. Urbani, et al.; Exp. Cell. Res. 219, 159 (1995) Abstract
Drug-induced apoptosis is not necessarily dependent on macromolecular synthesis or proliferation in the p53-negative human prostate cancer cell line PC-3: M.M. Borner, et al.; Cancer Res. 55, 2122 (1995) Abstract
TrkA neurogenic receptor regulates differentiation of neuroblastoma cells: W. Poluha, et al.; Oncogene 10, 185 (1995) Abstract
Coordinate regulation of G- and C strand length during new telomere synthesis: X. Fan and C.M. Price; Mol. Biol. Cell 8, 2145 (1997) Abstract; Full Text
Effect of aphidicolin on DNA methyltransferase in the nucleus: I. Suetake, et al.; Cell Struct. Funct. 23, 137 (1998) Abstract
Cytotoxicity of aphidicolin and its derivatives against neuroblastoma cells in vitro: synergism with doxorubicin and vincristine: M. Michaelis, et al.; Anticancer Drugs 11, 479 (2000) Abstract
Aphidicolin and bleomycin induced chromosome damage as biomarker of mutagen sensitivity: a twin study: B. Tedeschi, et al.; Mutat. Res. 546, 55 (2004) Abstract
 
 
ALX-350-017 Revised 18-Nov-08
Fumonisin B1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Tumor Promoters
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ALX-350-017-M001   1 mg 60.00 USD Add To Cart
ALX-350-017-M005   5 mg 245.00 USD Add To Cart
Product Specification
FORMULA: C34H59NO15
MW: 721.8
CAS NUMBER: 116355-83-0
MERCK INDEX: 14: 4289
RTECS: TZ8350000
SOURCE/HOST: Isolated from Fusarium moniliforme.
PURITY: ~98% (TLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (10mg/ml), methanol (5mg/ml), DMSO (20mg/ml) or acetonitrile.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE MUTAGENIC. MAY BE TERATOGENIC. MAY BE CARCINOGENIC. HARMFUL.

Product Description
Mycotoxin. Induces DNA damage in the liver and cancer. Inhibitor of sphingosine biosynthesis. Induces apoptosis. Activates Akt (protein kinase B; PKB), which leads to increased survival, inhibition of GSK-3β activity and post-translational stabilization of cyclin D1.
Product Specific Literature References
Inhibition of sphingolipid biosynthesis by fumonisins. Implications for diseases associated with Fusarium moniliforme: E. Wang, et al.; J. Biol. Chem. 266, 14486 (1991) Abstract; Full Text
Fumonisin B1 inhibits sphingosine (sphinganine) N-acyltransferase and de novo sphingolipid biosynthesis in cultured neurons in situ: A.H. Merrill Jr., et al.; J. Biol. Chem. 268, 27299 (1993) Abstract; Full Text
Biological activities of fumonisins, mycotoxins from Fusarium moniliforme, in jimsonweed (Datura stramonium L.) and mammalian cell cultures: H.K. Abbas, et al.; Toxicon 31, 345 (1993) Abstract
Fumonisins and Alternaria alternata lycopersici toxins: sphinganine analog mycotoxins induce apoptosis in monkey kidney cells: H. Wang, et al.; PNAS 93, 3461 (1996) Abstract
A potential mechanism for fumonisin B(1)-mediated hepatocarcinogenesis: cyclin D1 stabilization associated with activation of Akt and inhibition of GSK-3beta activity: D. Ramljak, et al.; Carcinogenesis 21, 1537 (2000) Abstract
Implications of apoptosis for toxicity, carcinogenicity, and risk assessment: fumonisin B(1) as an example: Y.P. Dragan, et al.; Toxicol. Sci. 61, 6 (2001), Review Abstract
Fumonisin B(1): oxidative status and DNA damage in rats: A.M. Domijan, et al.; Toxicology 232, 163 (2007) Abstract
 
 
ALX-350-032 Revised 08-Oct-08
Ingenol 3,20-dibenzoate
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Tumor Promoters
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ALX-350-032-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C34H36O7
MW: 556.7
CAS NUMBER: 59086-90-7
SOURCE/HOST: Semisynthetic.
PURITY: ≥96%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE CARCINOGENIC.

Product Description
Activates protein kinase C (PKC). Induces apoptosis. Anticancer agent. Shows potent antileukemic activity in the P388 mouse assay. Displays unusually high mouse ear inflammatory activity, even though the 20-hydroxy group is blocked with a benzoate ester. It appears likely that this high potency is due to metabolic cleavage of the 20-benzoate group, which releases the more potent ingenol 3-benzoate.
Product Specific Literature References
Antileukemic principles isolated from euphorbiaceae plants: S.M. Kupchan, et al.; Science 191, 571 (1976) Abstract
Zur Chemie des Ingcnols, II. Ester des Ingenols. und des A’-’-Isoingenols: B. Sorg & E. Hecker; Z. Naturforsch. 37b, 748 (1982)
Induction of thymocyte apoptosis by Ca2+-independent protein kinase C (nPKC) activation and its regulation by calcineurin activation: A. Asada, et al.; J. Biol. Chem. 273, 28392 (1998) Abstract
Ingenol esters induce apoptosis in Jurkat cells through an AP-1 and NF-kappaB independent pathway: M. Blanco-Molina, et al.; Chem. Biol. Interact. 8, 767 (2001) Abstract
 
 
ALX-350-057 Revised 20-Feb-08
Emodin
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SYNONYMS 6-Methyl-1,3,8-trihydroxyanthraquinone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-057-M025   25 mg 45.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 518-82-1
MERCK INDEX: 14: 3561
RTECS: CB7920600
SOURCE/HOST: Isolated from Frangula bark.
PURITY: ≥96% (HPLC)
APPEARANCE: Orange to red solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or 1N dilute aqueous ammonia; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: IRRITANT.

Product Description
Inhibitor of p56lck tyrosine kinase. Has mutagenic and genotoxic effects, mainly in bacterial systems. Anticancer agent. Exhibits anti-proliferative effects in various cancer cell lines by efficient induction of apoptosis. Has inhibitory effects on angiogenic and metastasis regulatory processes. Anti-inflammatory compound. Suppresses NF-κB activation. 
Product Specific Literature References
Emodin, a protein tyrosine kinase inhibitor from Polygonum cuspidatum: H. Jayasuriya, et al.; J. Nat. Prod. 55, 696 (1992) Abstract
Selective inhibition of the growth of ras-transformed human bronchial epithelial cells by emodin, a protein-tyrosine kinase inhibitor: T.C.K. Chan, et al.; BBRC 193, 1152 (1993) Abstract
Molecular mechanism of emodin action: transition from laxative ingredient to an antitumor agent: G. Srinivas, et al.; Med. Res. Rev. 27, 591 (2007), (Review) Abstract
 
 
ALX-350-069 Revised 02-Oct-08
Vincristine . sulfate